RasGRP1 Activators
The chemical class termed RasGRP1 activators encompasses compounds with diverse mechanisms of action, all converging on the modulation of RasGRP1, a key regulator of Ras signaling. These compounds play crucial roles in activating RasGRP1 and subsequently initiating downstream cellular responses. Phorbol 12-myristate 13-acetate (PMA) and its analog Phorbol 12,13-dibutyrate (PDBu) are classical activators that directly interact with the C1 domain of protein kinase C (PKC). Activated PKC phosphorylates and activates RasGRP1, initiating the Ras signaling pathway. Calyculin A, a potent protein phosphatase inhibitor, indirectly activates RasGRP1 by maintaining elevated phosphorylation levels, facilitating Ras activation and downstream signaling.
Forskolins activation of adenylate cyclase leads to increased cAMP levels, activating protein kinase A (PKA), which phosphorylates and activates RasGRP1. Conversely, Bisindolylmaleimide I and Bisindolylmaleimide IV, selective inhibitors of PKC, negatively regulate RasGRP1 by inhibiting PKC-mediated phosphorylation, reducing its efficacy in Ras activation. A23187, Calcimycin, and D-Mannitol influence RasGRP1 by modulating calcium levels. A23187, a calcium ionophore, directly activates RasGRP1 through binding to its EF-hand domain. Genistein, a tyrosine kinase inhibitor, indirectly modulates RasGRP1 by affecting upstream signaling events. Resveratrol, a polyphenol, activates AMP-activated protein kinase (AMPK), suggesting a potential role for metabolic regulation in RasGRP1 activity. In summary, the RasGRP1 activators class provides a comprehensive understanding of compounds that directly or indirectly influence RasGRP1, unraveling intricate regulatory mechanisms in the Ras signaling pathway. These compounds offer valuable insights into potential pharmacological interventions for modulating Ras-mediated cellular responses.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
PMA | 16561-29-8 | sc-3576 sc-3576A sc-3576B sc-3576C sc-3576D | 1 mg 5 mg 10 mg 25 mg 100 mg | $40.00 $129.00 $210.00 $490.00 $929.00 | 119 | |
Phorbol 12-myristate 13-acetate (PMA) activates protein kinase C (PKC) through its binding and interaction with the C1 domain. Activated PKC, in turn, phosphorylates and activates RasGRP1 by direct interaction, leading to the activation of the Ras signaling pathway and downstream cellular responses. | ||||||
Calyculin A | 101932-71-2 | sc-24000 sc-24000A | 10 µg 100 µg | $160.00 $750.00 | 59 | |
Calyculin A is a potent protein phosphatase inhibitor, particularly targeting PP1 and PP2A. By inhibiting phosphatases, calyculin A increases the phosphorylation status of signaling molecules, including RasGRP1. Elevated phosphorylation can enhance the activity of RasGRP1 and facilitate its role in activating Ras and downstream signaling pathways. | ||||||
Forskolin | 66575-29-9 | sc-3562 sc-3562A sc-3562B sc-3562C sc-3562D | 5 mg 50 mg 1 g 2 g 5 g | $76.00 $150.00 $725.00 $1385.00 $2050.00 | 73 | |
Forskolin activates adenylate cyclase, leading to increased levels of cAMP. Elevated cAMP activates protein kinase A (PKA), which, in turn, phosphorylates and activates RasGRP1. This activation promotes the exchange of GDP for GTP on Ras, leading to Ras activation and subsequent downstream signaling events. | ||||||
Bisindolylmaleimide I (GF 109203X) | 133052-90-1 | sc-24003A sc-24003 | 1 mg 5 mg | $103.00 $237.00 | 36 | |
Bisindolylmaleimide I is a potent and selective inhibitor of protein kinase C (PKC). Its action inhibits PKC-mediated phosphorylation of RasGRP1, negatively regulating its activity. In the absence of PKC-mediated phosphorylation, RasGRP1 may have reduced efficacy in activating Ras and downstream signaling pathways. | ||||||
A23187 | 52665-69-7 | sc-3591 sc-3591B sc-3591A sc-3591C | 1 mg 5 mg 10 mg 25 mg | $54.00 $128.00 $199.00 $311.00 | 23 | |
A23187 is a calcium ionophore that induces a rapid increase in intracellular calcium levels. Elevated calcium can activate RasGRP1 through direct binding to its EF-hand domain, leading to the activation of Ras and downstream signaling pathways. The calcium-dependent activation of RasGRP1 represents a crucial regulatory mechanism for initiating Ras-mediated cellular responses. | ||||||
Resveratrol | 501-36-0 | sc-200808 sc-200808A sc-200808B | 100 mg 500 mg 5 g | $60.00 $185.00 $365.00 | 64 | |
Resveratrol, a polyphenol, activates AMP-activated protein kinase (AMPK). Activated AMPK can phosphorylate and activate RasGRP1, contributing to the modulation of Ras signaling. This indirect activation through AMPK suggests a potential role for metabolic regulation in influencing RasGRP1 activity and downstream cellular responses. | ||||||
Phorbol-12,13-dibutyrate | 37558-16-0 | sc-202285 | 1 mg | $122.00 | 3 | |
Phorbol 12,13-dibutyrate (PDBu) is a diester derivative of phorbol and activates protein kinase C (PKC). Activated PKC phosphorylates RasGRP1, leading to its activation and subsequent initiation of the Ras signaling pathway. PDBu-induced activation of RasGRP1 represents a pharmacological means of influencing Ras-mediated cellular responses. | ||||||
Genistein | 446-72-0 | sc-3515 sc-3515A sc-3515B sc-3515C sc-3515D sc-3515E sc-3515F | 100 mg 500 mg 1 g 5 g 10 g 25 g 100 g | $26.00 $92.00 $120.00 $310.00 $500.00 $908.00 $1821.00 | 46 | |
Genistein is a tyrosine kinase inhibitor that can indirectly influence RasGRP1 activation. By inhibiting tyrosine kinases, genistein may modulate upstream signaling events that contribute to RasGRP1 activation. The specific tyrosine kinases involved in this modulation can vary, suggesting a nuanced regulatory role for genistein in influencing Ras-mediated cellular responses. | ||||||
Bisindolylmaleimide IV | 119139-23-0 | sc-3543 | 1 mg | $75.00 | 2 | |
Bisindolylmaleimide IV is another selective inhibitor of protein kinase C (PKC). Its action inhibits PKC-mediated phosphorylation of RasGRP1, negatively regulating its activity. The inhibition of PKC-dependent phosphorylation may result in reduced efficacy of RasGRP1 in activating Ras and downstream signaling pathways, providing a potential pharmacological means of modulating Ras-mediated cellular responses. | ||||||
D(−)Mannitol | 69-65-8 | sc-203020A sc-203020 | 50 g 100 g | $10.00 $19.00 | 2 | |
D-Mannitol, as an osmotic diuretic, can influence RasGRP1 indirectly. Changes in osmolarity can impact intracellular signaling events, including those leading to RasGRP1 activation. The specific mechanisms by which D-mannitol influences RasGRP1 require further investigation but may involve osmotically-induced alterations in cellular signaling cascades leading to the modulation of Ras-mediated cellular responses. | ||||||